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CAS No.: 210344-98-2

Z-IETD-FMK Catalog No. CSN13841

Synonyms: Z-IE(OMe)TD(OMe)-FMK;Caspase-8 Inhibitor;Granzyme B Inhibitor III

Z-IETD-FMK is a specific Caspase-8 inhibitor.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Caspase-8, belong to the Caspase family, is a cysteine protease which plays a key role in the initiation of apoptotic signaling pathway via death receptors. Z-IETD-FMK is a specific Caspase-8 inhibitor. Incubation with 20μM Z-IETD-FMK can inhibited the hsp27-comsuption-induced 30- and 20-kDa cleavage of Caspase-8, as well as showed partial inactivation of Caspase-3, in lysates of retinal cells, suggesting the selective inhibition of Caspase-8 by Z-IETD-FMK. Also, treatment with Z-IETD-FMK only dose-dependently decreased stress-induced caspase-3–like activity by incubation with hsp27 antibody, but not ischemia, AMPA or NMDA, in retinal cells^[1]. For Caspase-8 also a critical role during protozoan infection, blockade of caspase-8 by treatment with Z-IETD-FMK disturbed IL-2 production and induction of NF- B responses to TCR:CD3 engagement in T cell cultures. Injection of 0.4mg Z-IETD-FMK increased susceptibility to protozoan parasite Trypanosoma cruzi. infection in mice^[2].
作用机制Z-IETD-FMK is the substrate for caspase, which can bind to the active site to form an irreversible bond with the enzyme thus blocking it from further action.^[3]
动物研究
剂量
Mice: 10 mg/kg (co with doxorubicin)^[4]

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 10 mg/kg (co with doxorubicin)^[4]
给药途径	i.p.

[1] Tezel G, Wax MB, et al. Inhibition of caspase activity in retinal cell apoptosis induced by various stimuli in vitro. Invest Ophthalmol Vis Sci. 1999 Oct;40(11):2660-7.
[2] Silva EM, Guillermo LV, et al. Caspase-8 activity prevents type 2 cytokine responses and is required for protective T cell-mediated immunity against Trypanosoma cruzi infection. J Immunol. 2005 May 15;174(10):6314-21.
[3] Taimen P, Kallajoki M, et al. NuMA and nuclear lamins behave differently in Fas-mediated apoptosis. J Cell Sci. 2003 Feb 1;116(Pt 3):571-83.
[4] Shi J, Zhang L, et al. Downregulation of doxorubicin-induced myocardial apoptosis accompanies postnatal heart maturation. Am J Physiol Heart Circ Physiol. 2012;302(8):H1603-13.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5275 mL
- 7.6373 mL
- 15.2746 mL
- 5 mM
- 0.3055 mL
- 1.5275 mL
- 3.0549 mL
- 10 mM
- 0.1527 mL
- 0.7637 mL
- 1.5275 mL

技术信息

CAS号

210344-98-2

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H43FN4O11

运输

蓝冰

分子量

654.68

别名

Z-IE(OMe)TD(OMe)-FMK;Caspase-8 Inhibitor;Granzyme B Inhibitor III;MDK-4982;Z-Ile-Glu(OMe)-Thr-Asp(OMe)-CH₂F

溶解度

DMSO	79.0 mg/mL (120.7 mM)
Water	insoluble

动物实验配方

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